151213-42-2

151213-43-3

151213-42-2

The general procedure for the synthesis of (4aR,7aR)-octahydro-6-(phenylmethyl)-1H-pyrrolo[3,4-b]pyridine from (4aR,7aR)-octahydro-1H-pyrrolo[3,4-b]pyridine is as follows: 19.4 g (0.09 mol) of (R,R)-8-benzyl-2,8-diazabicyclo[4.3.0]nonane was dissolved in methanol with the addition of 3.96 g of 5% palladium/activated carbon catalyst and hydrogenated at 90 °C and 130 °C for 5 hours. Upon completion of the reaction, the catalyst was removed by filtration and the catalyst was washed with methanol. The filtrate was concentrated under vacuum and the residue was directly distilled without fractionation. A final product of 9.61 g was obtained in 85% yield of the theoretical value. The boiling point of the product was 45-58°C/0.08 mbar.